Discovery of [C-11]MK-8056: A Selective PET Imaging Agent for the Study of mGluR(2) Negative Allosteric Modulators

James J. J. Perkins,Paul McQuade,Christopher J. J. Bungard,Tracy L. L. Diamond,Liza T. T. Gantert,Anthony L. L. Gotter, Barbara Hanney, Ivory D. D. Hills, Danielle M. M. Hurzy,Aniket Joshi, Jonathan T. T. Kern, Kelly-Ann S. Schlegel,Jesse J. J. Manikowski,Zhaoyang Meng, Julie A. A. O'Brien,Anthony J. J. Roecker,Sean M. M. Smith,Jason M. M. Uslaner,Eric Hostetler, Robert S. S. Meissner

ACS MEDICINAL CHEMISTRY LETTERS（2023）

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摘要

Modification of potent, selective metabotropic glutamatereceptor2 negative allosteric modulator (mGluR(2) NAM) led to a seriesof analogues with excellent binding affinity, lipophilicity, and suitablephysicochemical properties for a PET tracer with convenient chemicalhandles for incorporation of a C-11 or F-18 radiolabel.[C-11]MK-8056 was synthesized and evaluated in vivo and demonstrated appropriate affinity, selectivity, and physicochemicalproperties to be used as a positron emission tomography tracer formGluR(2).

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关键词

MK-8056, Metabotropic Glutamate Receptor 2, Negative Allosteric Modulator, Positron Emission Tomography, Radiosynthesis

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